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Amides derived from heteroaromatic amines and selected steryl hemiesters

机译:Amides derived from heteroaromatic amines and selected steryl hemiesters

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摘要

The current interest of the team has been focused on investigation of novel amides with potential cyto-toxicity. The presented series of compounds was synthesized from selected steryl hemiesters and heteroaromatic amines. The synthetic protocol was designed in a simple and economic way, and divided into several general methodologies applicable to the compounds synthesized. The cytotoxicity was tested on cells derived from human T-lymphoblastic leukemia, breast adenocarcinoma and cervical cancer, and compared with tests on normal human fibroblasts. Most of the lanosterol-based compounds (3-5 and 7-10) showed medium to good cytotoxicity, while only two derivatives of cholesterol (18 and 19) showed medium cytotoxicity on human T-lymphoblastic leukemia cell line. The compounds 8 and 9 displayed the reasonable cytotoxicity among this series of amides, tested on the cell lines of T-lymphoblastic leukemia 14.5 ±0.4 muM (8) and 18.5 ±3.9 muM (9), breast adenocarcinoma 19.5 ± 2.1 muM (8) and 23.1 ±4.0 muM (9) and cervical cancer 24.8 ± 5.3 uM (8) and 29.1 ±4.7 uM (9). Only the compound 8 was adequately less active on normal human fibroblasts (40.4 ± 11.1 muM).

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